Ranganatha, S. R. and Malviya, Manish and Sunil Kumar, Y. C. and Vinaya, K. and Prasanna, D. S. and Subhash, M. N. and Rangappa, K. S. (2009) Effect of novel amino acids and dipeptides substituted 3-morpholino arecoline derivatives as muscarinic receptor 1 agonists in alzheimer's dementia models. INTERNATIONAL JOURNAL OF PEPTIDE RESEARCH AND THERAPEUTICS, 15 (4). pp. 323-337. ISSN 1573-3904
Full text not available from this repository. (Request a copy)Abstract
A series of novel, potent and selective muscarinic receptor 1 agonists (M1 receptor agonists) that employ a key N-substituted morpholine arecoline moiety has been synthesized as part of research effort for the therapy of Alzheimer's diseases. The ester group of arecoline (which is reported as mucarinic agonist) has been replaced by N-substituted morpholine ring. The structure activity relationship reveals that the increase in lipophilic carbon chain on the nitrogen atom of the morpholine ring increases the affinity of M1 receptor. In the present study, we are reporting N-amino acid substituted 9(a-k) and dipeptides substituted 10(a-j) and 11(a-j) morpholino arecoline derivatives, along with their in vitro muscarinic binding studies by using H-3]QNB and also in vivo evaluation of memory and learning in male Wistar rats (passive avoidance test plus maze studies) as M1 receptor agonist. Some molecules from the dipeptide series (10b, 10c and 10j) showed potent M1 receptor agonist activity. Other derivatives also showed considerable M1 receptor binding affinity.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | Alzheimer's disease; M1 agonists; Morpholino arecolines; Peptide conjugates |
| Subjects: | C Chemical Science > Chemistry |
| Divisions: | Department of > Chemistry |
| Depositing User: | Users 19 not found. |
| Date Deposited: | 13 Aug 2019 05:28 |
| Last Modified: | 13 Aug 2019 05:28 |
| URI: | http://eprints.uni-mysore.ac.in/id/eprint/6304 |
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